Ezolong powder for solution for injection or infusion 40 mg vial No. 10

Instructions Ezolong powder for solution for injection or infusion 40 mg vial No. 10

Composition

active ingredient: esomeprazole;

1 vial contains 42.60 mg of esomeprazole sodium, equivalent to 40 mg of esomeprazole;

excipients: disodium edetate (Trilon B), sodium hydroxide.

Dosage form

Powder for solution for injection or infusion.

Main physicochemical properties: porous and homogeneous lyophilized powder of white or almost white color.

Pharmacotherapeutic group

Drugs for the treatment of peptic ulcer and gastroesophageal reflux disease. Proton pump inhibitors. Esomeprazole. ATC code A02B C05.

Pharmacological properties

Pharmacodynamics.

Esomeprazole is the S-isomer of omeprazole, which inhibits gastric acid secretion by a specific, targeted mechanism of action. It is a specific inhibitor of the parietal cell acid pump. Both the R- and S-isomers of omeprazole have similar pharmacological activities.

Mechanism of action. Esomeprazole is a weak base. After entering the body, esomeprazole is concentrated and converted to the active form in the highly acidic environment of the secretory tubules of parietal cells. It is there that there is a need to inhibit the enzyme H+K+-ATPase - the "proton pump". This leads to inhibition of both basal and stimulated acid secretion in the stomach.

Effect on gastric secretion. After 5 days of oral administration of 20 mg and 40 mg esomeprazole, gastric pH above 4 was maintained for an average of 13 hours and 17 hours over a 24-hour period, respectively, in patients with symptomatic gastroesophageal reflux disease (GERD). The extent of the therapeutic effect was independent of the route of administration of esomeprazole, either orally or intravenously.

After evaluating the area under the pharmacokinetic concentration-time curve (AUC) as a proxy for drug concentration, a relationship between acid suppression and exposure following oral administration of esomeprazole was demonstrated.

When esomeprazole was administered intravenously to healthy volunteers at a dose of 80 mg as a bolus infusion over 30 minutes followed by a continuous intravenous infusion at a rate of 8 mg/hour for 23.5 hours, gastric pH levels above 4 and above 6 were maintained for an average of 21 hours and 11–13 hours over a 24-hour period, respectively.

Therapeutic significance of the acid-suppressing effect: With oral administration of esomeprazole at a dose of 40 mg, approximately 78% of patients with reflux esophagitis recover after 4 weeks and 93% after 8 weeks of treatment.

According to the published results of a randomized, double-blind, placebo-controlled clinical trial in patients with endoscopically proven peptic ulcer class Ia, Ib, IIa or IIb (9%, 43%, 38% and 10% respectively) according to Forest, a decrease in the frequency of rebleeding in the first 72 hours was noted by almost 2 times against the background of the use of esomeprazole intravenously compared with.

Other effects related to the inhibition of acid secretion. During treatment with antisecretory agents, the serum gastrin level increases. This is a physiological response to the reduction in acid secretion. The level of chromogranin A (CgA) also increases due to the reduction in gastric acidity.

In some patients, during long-term treatment with oral forms of esomeprazole, an increase in the number of enterochromaffin-like cells was noted, possibly associated with an increase in gastrin levels. There was also a slight increase in the frequency of formation of glandular cysts in the gastric mucosa. These changes are a physiological consequence of pronounced inhibition of gastric juice secretion, are benign and reversible in nature.

Decreased gastric acidity from any cause, including proton pump inhibitors (PPIs), leads to an increase in the number of bacteria normally present in the gastrointestinal tract in the stomach. PPI treatment may slightly increase the risk of gastrointestinal infections, such as Salmonella and Campylobacter, and in hospitalized patients, possibly due to Clostridium difficile.

Children

Results from studies in pediatric patients show that doses of esomeprazole 0.5 mg/kg and 1.0 mg/kg in infants < 1 month and 1-11 months of age, respectively, reduce the mean percentage of time with esophageal pH < 4.

The safety profile of the drug was similar to that observed in adults.

Pharmacokinetics.

Distribution: Esomeprazole is 97% bound to plasma proteins. The apparent volume of distribution at steady state in healthy volunteers is approximately 0.22 l/kg body weight.

Metabolism: Esomeprazole is completely metabolized by the cytochrome P450 (CYP) system. The main part of the metabolism of esomeprazole depends on the polymorphic CYP2C19, which is responsible for the formation of the hydroxy- and desmethyl metabolites of esomeprazole. The remaining metabolism is provided by another specific isoform, CYP3A4, which is responsible for the formation of esomeprazole sulfone, the main metabolite in blood plasma.

Total plasma clearance is approximately 17 l/h after a single dose and approximately 9 l/h after repeated administration. The plasma elimination half-life is approximately 1.3 h after repeated once daily administration. AUC increases with repeated administration of esomeprazole. This increase is dose-dependent and results in a non-linear relationship between dose and AUC after repeated administration. This time- and dose-dependence is due to a decrease in first-pass metabolism and systemic clearance, likely due to inhibition of the CYP2C19 enzyme by esomeprazole and/or its sulfone metabolite.

Elimination: Esomeprazole is completely eliminated from the blood plasma between doses, and there is no tendency for its accumulation in the body when administered once daily.

After repeated intravenous administration of 40 mg, the mean maximum plasma concentration is approximately 13.6 μmol/l. The mean maximum plasma concentration after corresponding oral doses is approximately 4.6 μmol/l. A smaller increase (approximately 30%) in total exposure is observed with intravenous administration compared with oral administration. A linear dose-dependent increase in exposure was observed when esomeprazole was administered as an intravenous infusion over 30 minutes (40 mg, 80 mg or 120 mg) followed by a continuous infusion (4 mg/h or 8 mg/h) for 23.5 hours.

The main metabolites of esomeprazole do not affect gastric secretion. Almost 80% of an oral dose of esomeprazole is excreted as metabolites in the urine, the rest in the feces. Less than 1% of the parent compound is excreted in the urine.

Special populations. Approximately 2.9 ± 1.5% of the population lack a functional CYP2C19 enzyme and are referred to as poor metabolisers. In these individuals, the metabolism of esomeprazole is likely to be predominantly catalysed by CYP3A4. After multiple oral doses of 40 mg esomeprazole once daily, the mean total exposure was approximately 100% higher in poor metabolisers than in subjects with a functional CYP2C19 enzyme (extensive metabolisers). The mean maximum plasma concentration was increased by approximately 60%. Similar differences were observed with intravenous administration of esomeprazole. These findings do not require any changes in the dosage of esomeprazole.

The metabolism of esomeprazole is slightly altered in the elderly (71-80 years).

After a single oral dose of 40 mg esomeprazole, the mean total exposure in women is approximately 30% higher than in men. No gender differences were observed with repeated once daily dosing. Similar differences were observed with intravenous administration of esomeprazole. These findings do not impact the posology of esomeprazole.

The metabolism of esomeprazole may be impaired in patients with mild or moderate hepatic impairment. In patients with severe hepatic impairment, the rate of metabolism is reduced, resulting in a doubling of the total exposure to esomeprazole. Therefore, in patients with GERD and severe hepatic impairment, the maximum dose of 20 mg should not be exceeded. In the case of bleeding ulcers and severe hepatic impairment, after an initial bolus dose of 80 mg, a continuous intravenous infusion of up to 4 mg/hour for 71.5 hours may be sufficient. Esomeprazole or its major metabolites do not show a tendency to accumulate when administered once daily.

Studies in patients with reduced renal function have not been conducted. Since the kidneys are responsible for the excretion of esomeprazole metabolites, but not the parent compound, no changes in metabolism are expected in patients with impaired renal function.

Indication

Adults

Antisecretory therapy when oral administration is not possible, for example:

gastroesophageal reflux disease in patients with esophagitis and/or severe reflux symptoms;

treatment of stomach ulcers associated with nonsteroidal anti-inflammatory drug (NSAID) therapy;

prevention of gastric and duodenal ulcers associated with NSAID therapy in patients at risk.

Prevention of rebleeding in patients after endoscopic treatment of acute bleeding due to gastric or duodenal ulcer.

Children aged 1 to 18 years:

Antisecretory therapy when oral administration is not possible, for example:

GERD in patients with erosive reflux esophagitis and/or severe reflux symptoms.

Contraindication

Hypersensitivity to esomeprazole, other substituted benzimidazoles or to any of the excipients of the medicinal product.

The drug Ezolong® should not be used simultaneously with nelfinavir, atazanavir (see section “Interaction with other medicinal products and other types of interactions”).

Interaction with other medicinal products and other types of interactions

Interaction studies have only been conducted in adults.

Medicinal products whose absorption is dependent on pH. Inhibition of gastric secretion by esomeprazole and other PPIs may lead to a decrease or increase in the absorption of medicinal products whose absorption is dependent on the pH of the gastric juice. As with other medicinal products that reduce gastric acidity, the absorption of such medicinal products as ketoconazole, itraconazole and erlotinib may be reduced and the absorption of digoxin may be increased during the use of esomeprazole. When omeprazole (20 mg daily) was co-administered with digoxin in healthy volunteers, the bioavailability of digoxin increased by 10% (up to 30% in two out of ten participants). Toxic effects of digoxin have been observed rarely. However, caution should be exercised when using high doses of esomeprazole in elderly patients. Monitoring of digoxin concentrations in the patient's blood should be intensified.

Interaction of omeprazole with some protease inhibitors. The clinical significance and mechanisms of these interactions are not always known. The increase in gastric pH during omeprazole therapy may alter the absorption of protease inhibitors. Other possible mechanisms of interaction include inhibition of CYP2C19. Decreased serum levels of atazanavir and nelfinavir have been observed with concomitant use of omeprazole, therefore concomitant use of these drugs is not recommended. Co-administration of omeprazole (40 mg once daily) with atazanavir 300 mg/ritonavir 100 mg in healthy volunteers resulted in a significant decrease in atazanavir exposure (approximately 75% decrease in AUC, Cmax and Cmin). Increasing the dose of atazanavir to 400 mg did not compensate for the effect of omeprazole on atazanavir exposure. Co-administration of omeprazole (20 mg daily) with atazanavir 400 mg/ritonavir 100 mg in healthy volunteers decreased atazanavir exposure by approximately 30% compared to the exposure observed with atazanavir 300 mg/ritonavir 100 mg once daily without omeprazole 20 mg daily. Co-administration of omeprazole (40 mg daily) decreased the mean AUC, Cmax, and Cmin of nelfinavir by 36–39% and the mean AUC, Cmax, and Cmin of the pharmacologically active metabolite M8 by 75–92%.

Increased serum concentrations of saquinavir (co-administered with ritonavir) (80-100%) were observed with concomitant use of omeprazole (40 mg daily). Omeprazole 20 mg daily had no effect on the exposure of darunavir (co-administered with ritonavir) and amprenavir (in combination with ritonavir). Esomeprazole 20 mg daily had no effect on the exposure of amprenavir (in combination with ritonavir or alone). Omeprazole 40 mg daily did not alter the exposure of lopinavir (in combination with ritonavir). Due to the similarity of pharmacodynamic effects and pharmacokinetic properties of omeprazole and esomeprazole, concomitant use of esomeprazole and atazanavir is not recommended, and concomitant use of esomeprazole and nelfinavir is contraindicated.

Drugs metabolized by CYP2C19

Esomeprazole inhibits CYP2C19, the main enzyme that metabolizes esomeprazole. Therefore, when esomeprazole is combined with drugs that are metabolized by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, the plasma concentrations of these drugs may increase and a dose reduction may be required. Concomitant oral administration of 30 mg esomeprazole resulted in a 45% decrease in the clearance of the CYP2C19 substrate diazepam. Concomitant oral administration of 40 mg esomeprazole and phenytoin resulted in a 13% increase in the trough plasma concentration of phenytoin in patients with epilepsy. It is recommended to monitor the plasma concentration of phenytoin when initiating and stopping esomeprazole therapy.

Omeprazole (40 mg once daily) increased the Cmax and AUCτ of voriconazole (a CYP2C19 substrate) by 15% and 41%, respectively.

When concomitant oral esomeprazole 40 mg was administered to patients taking warfarin in a clinical trial, the bleeding time remained within the acceptable range. However, in the post-marketing period, a few isolated cases of clinically significant increases in MCH have been reported with oral esomeprazole when these drugs were used concomitantly. Monitoring is recommended at the beginning and end of concomitant use of esomeprazole and warfarin or other coumarin derivatives.

Increased serum levels of tacrolimus have been reported with concomitant use of esomeprazole.

Increased monitoring of tacrolimus concentrations and renal function (creatinine clearance) is necessary and, if necessary, the tacrolimus dose should be adjusted.

Omeprazole, like esomeprazole, is an inhibitor of CYP2C19. In a cross-over study in healthy volunteers, the use of omeprazole at a dose of 40 mg resulted in an increase in Cmax and AUC of cilostazol by 18% and 26%, respectively, and of one of its active metabolites by 29% and 69%.

Esomeprazole has been shown to have no clinically significant effect on the pharmacokinetics of amoxicillin or quinidine.

Studies evaluating the concomitant use of esomeprazole and naproxen or rofecoxib did not reveal any clinically significant pharmacokinetic interactions in short-term studies.

In vivo interaction studies with the high dose intravenous formulation (80 mg + 8 mg/hour) have not been performed. The effect of esomeprazole on drugs metabolized by CYP2C19 may be more pronounced with this regimen and patients should be closely monitored for adverse reactions during the three-day intravenous administration period.

Results of studies in healthy volunteers showed a pharmacokinetic (PK)/pharmacodynamic (PD) interaction between clopidogrel (300 mg loading dose/75 mg daily maintenance dose) and esomeprazole (40 mg daily), resulting in a mean 40% reduction in exposure to the active metabolite of clopidogrel, resulting in a mean 14% reduction in maximal inhibition of (ADP-induced) platelet aggregation.

When clopidogrel was administered with a fixed-dose combination of esomeprazole 20 mg + ASA 81 mg compared to clopidogrel monotherapy in a study in healthy volunteers, there was a decrease in exposure to the active metabolite of clopidogrel by almost 40%. However, the maximum inhibition of (ADP-induced) platelet aggregation in these patients was similar in the clopidogrel and clopidogrel + combination (esomeprazole + ASA) groups.

Both observational and clinical studies have yielded conflicting data on the clinical consequences of esomeprazole PK/PD interactions in serious cardiovascular events.

The mechanism of interaction with methotrexate is unknown. Methotrexate levels have been increased in some patients when used with PPIs. Temporary discontinuation of esomeprazole may be necessary when high doses of methotrexate are used.

Effect of other medicinal products on the pharmacokinetics of esomeprazole

Esomeprazole is metabolised by CYP2C19 and CYP3A4. Concomitant oral administration of esomeprazole and the CYP3A4 inhibitor clarithromycin (500 mg twice daily) resulted in a doubling of esomeprazole AUC. Concomitant administration of esomeprazole and a combined CYP2C19 and CYP3A4 inhibitor may result in a more than two-fold increase in esomeprazole exposure. The CYP2C19 and CYP3A4 inhibitor voriconazole increased the AUCτ of omeprazole by 280%. Dose adjustment of esomeprazole is not always necessary in these situations. However, it may be necessary in patients with severe hepatic impairment and in cases where long-term treatment is indicated.

Drugs that can induce CYP2C19 or CYP3A4 or both of these enzymes (rifampicin and St. John's wort) may reduce the serum concentration of esomeprazole by increasing its metabolism.

Application features

In case of any alarming symptoms (e.g. significant unexpected weight loss, recurrent vomiting, dysphagia, hematemesis or melena) and if gastric ulcer is suspected or present, malignant disease should be excluded, as Ezolong® may mask symptoms and delay diagnosis.

PPI therapy may slightly increase the risk of gastrointestinal infections, such as those caused by Salmonella and Campylobacter (see section 5.1).

The use of esomeprazole with atazanavir is not recommended (see section 4.5). If the combination of atazanavir with a PPI is considered necessary, close monitoring of the patient is recommended and the dose of atazanavir should be increased to 400 mg with 100 mg ritonavir; the dose of esomeprazole should not exceed 20 mg.

Esomeprazole, like all acid-blocking drugs, may inhibit the absorption of vitamin B12 (cyanocobalamin) due to hypo- or achlorhydria. This should be taken into account in patients with reduced body stores or risk factors for impaired vitamin B12 absorption during long-term therapy.

Esomeprazole is a CYP2C19 inhibitor. When initiating and ending therapy with esomeprazole, the possibility of interactions with drugs metabolized by CYP2C19 should be considered. An interaction between clopidogrel and omeprazole has been reported (see section 4.5). The clinical significance of this interaction is not fully understood. As a precautionary measure, concomitant use of esomeprazole and clopidogrel is not recommended.

Cases of severe hypomagnesemia have been reported in patients taking PPIs such as esomeprazole for at least 3 months, and in most cases for a year. Hypomagnesemia can have serious manifestations such as fatigue, tetany, delirium, seizures, dizziness, and ventricular arrhythmias, but its development may be gradual and go unnoticed. In most patients with hypomagnesemia, the condition improved after magnesium replacement therapy and discontinuation of the PPI.

PPIs, especially when used at high doses and for long periods (> 1 year), may slightly increase the risk of hip, wrist, and spine fractures, mainly in elderly patients or those with other risk factors. Review studies suggest that PPIs may increase the overall risk of fractures by 10-40%. This increase may be partly due to other risk factors. Patients at risk of osteoporosis should be treated according to current clinical guidelines and should receive adequate vitamin D and calcium.

The use of PPIs has been associated with very rare cases of subacute cutaneous systemic lupus erythematosus (SLE). If lesions occur, especially in sun-exposed areas of the skin, accompanied by arthralgia, the patient should seek medical attention immediately and discontinue Ezolong®. The treating physician should consider the appropriateness of using Ezolong®, taking into account previous experience with PPIs, which has been associated with the development of SLE.

Serious cutaneous adverse reactions (SCARs), such as erythema multiforme (EM), Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) and drug reaction with eosinophilia and systemic symptoms (DRESS), which can be life-threatening, have been reported very rarely in association with esomeprazole treatment.

Patients should be informed about the signs and symptoms of severe skin reaction (ME/SSD/TEN/DRESS) and to seek immediate medical attention from their physician if any signs or symptoms occur.

Esomeprazole should be discontinued immediately if signs and symptoms of serious skin reactions appear and additional medical attention/careful monitoring should be provided as necessary.

Patients with ME/SSD/TEN/DRESS should avoid reinfection.

Acute tubulointerstitial nephritis (TIN) has been observed in patients taking esomeprazole and naproxen-containing products and may occur at any time during therapy with Ezolong®.

Acute tubulointerstitial nephritis may progress to renal failure. Ezolong® should be discontinued if TIN is suspected and appropriate treatment should be initiated immediately.

Impact on laboratory test results

Elevated CgA levels may interfere with the diagnosis of neuroendocrine tumors. To avoid this, esomeprazole should be temporarily discontinued for at least five days before CgA measurement. If CgA and gastrin levels have not returned to the control range after the initial measurement, the measurement should be repeated 14 days after discontinuation of PPI treatment.

Each vial of this medicine contains less than 1 mmol (23 mg) sodium/dose, i.e. essentially sodium-free.

Use during pregnancy or breastfeeding

Pregnancy

Data on the use of esomeprazole during pregnancy are limited. A somewhat larger number of epidemiological studies on the use of the racemic mixture of omeprazole during pregnancy indicate no risk of congenital malformations and no toxicity of the drug to the fetus.

Animal studies with esomeprazole do not indicate direct or indirect harmful effects of the drug on embryonal/fetal development.

Animal studies of the racemic mixture do not indicate direct or indirect harmful effects with respect to pregnancy, childbirth or postnatal development. Ezolong® should be administered with caution to pregnant women.

A moderate amount of data on pregnant women (300 to 1000 pregnancy outcomes) indicate no risk of congenital malformations or foetal/neonatal toxicity of esomeprazole.

The results of animal studies indicate the absence of direct or indirect harmful effects of the medicinal product on reproductive function due to its toxic effect.

Breastfeeding period

It is not known whether esomeprazole passes into breast milk. There is insufficient information on the effects of esomeprazole on newborns/infants. Therefore, Ezolong® should not be used during breastfeeding.

Fertility

Animal studies of the racemic mixture of omeprazole indicate no effect of omeprazole on fertility when administered orally.

Ability to influence reaction speed when driving vehicles or other mechanisms

Esomeprazole has minor influence on the ability to drive and use machines. Adverse reactions such as dizziness (uncommon) and blurred vision (uncommon) have been reported (see section 4.8). If such disorders occur, patients should not drive or use machines.

Method of administration and doses

Dosage

Adults

Antisecretory therapy when oral administration is not possible

In the treatment of gastric ulcers caused by the use of NSAIDs, the usual dose is 20 mg once a day. For the prevention of gastric and duodenal ulcers caused by NSAID therapy, patients at risk should be prescribed the drug at a dose of 20 mg once a day.

Treatment with intravenous medication is usually short-term, and patients should be switched to oral medication as soon as possible.

Short-term maintenance of hemostasis and prevention of rebleeding in patients after endoscopic treatment of acute bleeding due to gastric or duodenal ulcer

After therapeutic endoscopy of acute bleeding gastric or duodenal ulcers, administer 80 mg of the drug as a bolus infusion lasting 30 minutes, then continue the drug as a continuous intravenous infusion at a rate of 8 mg/hour for 3 days (72 hours).

After parenteral treatment, therapy should be continued with oral agents that suppress acid secretion.

Method of application

Instructions for preparing the reconstituted solution are provided in this section below (“Instructions for use, handling and disposal (where applicable)”).

Infusions

Dose 40 mg

The reconstituted solution should be administered as an intravenous infusion over 10–30 minutes.

Dose 20 mg

Administer half of the reconstituted solution as an intravenous infusion over 10–30 minutes. Discard any unused solution.

Dose 80 mg

The reconstituted solution should be administered as a continuous intravenous infusion over 30 minutes.

Dose 8 mg/h

The reconstituted solution should be administered as a continuous intravenous infusion over 71.5 hours (calculated infusion rate 8 mg/hour; the shelf life of the reconstituted solution is indicated in the “Expiration Date” section).

Injections

Dose 40 mg

5 ml of the reconstituted solution (8 mg/ml) is administered as an intravenous injection over at least 3 minutes.

Dose 20 mg

2.5 ml or half of the reconstituted solution (8 mg/ml) should be administered as an intravenous injection over at least 3 minutes. Discard any unused solution.

Kidney dysfunction

No dose adjustment is necessary for patients with renal impairment. As experience in patients with severe renal impairment is limited, such patients should be treated with caution (see section 5.2).

Liver dysfunction

GERD: No dose adjustment is required in patients with mild or moderate hepatic impairment. Patients with severe hepatic impairment should not exceed a maximum dose of 20 mg (see section 5.2).

Bleeding ulcers: No dose adjustment is required in patients with mild or moderate hepatic impairment; in patients with severe hepatic impairment, after an initial bolus dose of 80 mg Ezolong® for infusion, a continuous intravenous infusion of 4 mg/hour for 71.5 hours may be sufficient (see Pharmacokinetics).

Elderly patients

No dose adjustment is required.

Children

Children aged 1 to 18 years

As a means of suppressing gastric secretion when oral administration of the drug is not possible

For patients who cannot take the drug orally, the drug can be administered parenterally once a day during the complete treatment period for GERD (doses are listed in the table below).

Treatment with intravenous medication is usually short-term. Patients should be switched to oral medication as soon as possible.

Recommended doses of esomeprazole for intravenous administration

Method of application

Instructions for preparing the reconstituted solution are provided in this section below (“Instructions for use, handling and disposal (where applicable)”).

Injections

Dose 40 mg

5 ml of the reconstituted solution (8 mg/ml) should be administered as an intravenous injection over at least 3 minutes.

Dose 20 mg

2.5 ml or half of the reconstituted solution (8 mg/ml) should be administered as an intravenous injection over at least 3 minutes. Discard any unused solution.

Dose 10 mg

1.25 ml of the reconstituted solution (8 mg/ml) should be administered as an intravenous injection over at least 3 minutes. Discard any unused solution.

Infusions

Dose 40 mg

The reconstituted solution should be administered as an intravenous infusion over 10–30 minutes.

Dose 20 mg

Administer half of the reconstituted solution as an intravenous infusion over 10–30 minutes. Discard any unused solution.

Dose 10 mg

Administer one-quarter of the reconstituted solution as an intravenous infusion over 10–30 minutes. Discard any unused solution.

The reconstituted solution should be inspected visually for particulate matter and discoloration prior to administration. Only clear solutions should be used. The solution is for single use only.

If the entire reconstituted vial contents are not required, the unused solution should be disposed of in accordance with local requirements.

Solution for injection 40 mg

Prepare a solution for injection (8 mg/mL) by adding 5 mL of 0.9% sodium chloride intravenous solution to a vial of esomeprazole 40 mg.

The reconstituted solution for injection is clear and colorless to slightly yellowish.

Solution for infusion 40 mg

Prepare the infusion solution by dissolving the contents of 1 vial of esomeprazole 40 mg in 100 ml of 0.9% sodium chloride for intravenous use.

Solution for infusion 80 mg

Prepare the infusion solution by dissolving the contents of 2 vials of esomeprazole 40 mg in 100 ml of 0.9% sodium chloride for intravenous use.

The reconstituted solution for infusion is clear and colourless or slightly yellowish.

Children.

It is used in children over 1 year of age as an antisecretory therapy when oral administration of the drug is not possible.

Overdose

Experience with intentional overdose is very limited to date. Symptoms following oral administration of 280 mg were gastrointestinal symptoms and weakness. A single oral dose of 80 mg esomeprazole and intravenous administration of 308 mg esomeprazole over 24 hours were without sequelae. No specific antidote is known. Esomeprazole is highly bound to plasma proteins and is therefore poorly dialysable. As with any overdose, symptomatic treatment and general supportive measures should be given.

Adverse reactions

The following adverse drug reactions have been identified or suspected in the clinical trial program of esomeprazole with oral or intravenous administration, as well as during post-marketing surveillance with oral administration. The reactions are categorized by frequency: very common (≥1/10); common (≥1/100 - <1/10); uncommon (≥1/1000 - <1/100); rare (≥1/10000 - <1/1000); very rare (<1/10000); frequency unknown (cannot be estimated from the available data).

Organ system classes	Adverse reactions
Blood and lymphatic system disorders	Rare: leukopenia, thrombocytopenia. Very rare: agranulocytosis, pancytopenia.
On the part of the immune system	Rare: hypersensitivity reactions, such as fever, angioedema and anaphylactic reactions/shock.
Metabolism and nutrition	Uncommon: peripheral oedema. Rare: hyponatremia. Frequency not known: hypomagnesemia (see section 4.4); severe hypomagnesemia may correlate with hypocalcemia. Hypomagnesemia may also be associated with hypokalemia.
Mental disorders	Uncommon: insomnia. Rare: agitation, confusion, depression. Very rare: aggression, hallucinations.
From the nervous system	Common: headache. Uncommon: dizziness, paraesthesia, drowsiness. Rare: taste disturbance Specifications Characteristics Active ingredient Esomeprazole Adults Can ATC code A DRUGS AFFECTING THE DIGESTIVE SYSTEM AND METABOLISM; A02 DRUGS FOR THE TREATMENT OF ACID-RELATED DISEASES; A02B DRUGS FOR THE TREATMENT OF PEPTIC ULCER AND GASTRO-ESOPHAGIAL REFLUX DISEASE; A02B C Proton pump inhibitors; A02B C05 Esomeprazole Country of manufacture Portugal Diabetics Can Dosage 40 мг Drivers With caution For allergies With caution For children From the 1st year Form Vials with dry contents Method of application Injections Nursing It is impossible. Pregnant It is impossible. Primary packaging bottle Producer Organosyn Lifesciences Ltd Quantity per package 10 bottles Trade name Esolong Vacation conditions By prescription Reviews There are no reviews for this product. + Add review Write a review Ezolong powder for solution for injection or infusion 40 mg vial No. 10 My mark: Continue There are no reviews for this product, be the first to leave your review. Answers & questions Add your question and we will answer as soon as possible. + Ask a question Ask a question Add your question and we will answer as soon as possible. * Your question Continue No questions about this product, be the first and ask your question. You are watched new Hit Windi gas vent tube for babies No. 10 In stock 0 592.99 грн. Add to Cart new Hit KlinTon ear spray solution bottle 15 ml In stock 0 291.16 грн. Add to Cart